Medicinal Chemistry: Drug Synthesis and Optimization

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Questions and Answers

What is the primary goal of development synthesis in medicinal chemistry?

  • To synthesize a clinical candidate as efficiently and safely as possible (correct)
  • To identify the pharmacophore of a lead compound
  • To modify natural products with similar structural motifs
  • To synthesize lots of analogs as efficiently as possible

What approach involves identifying compounds with similar structures and modifying the synthetic route to apply to target compounds?

  • Convergent synthesis
  • Modification of natural products
  • Identification of compounds with similar structures (correct)
  • Retrosynthetic analysis

What is the advantage of convergent synthesis over linear synthesis?

  • It results in a higher overall yield (correct)
  • It results in a lower overall yield
  • It is more complex and difficult to design
  • It requires more starting materials

What is the primary consideration when selecting a synthetic route?

<p>The yield and purity of the products (D)</p>
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What is the purpose of retrosynthetic analysis in medicinal chemistry?

<p>To design a synthetic route for a target compound (A)</p>
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What is the goal of hit to lead optimization in medicinal chemistry?

<p>To optimize a lead compound for pharmacodynamics and pharmacokinetics (D)</p>
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What is the main difference between MK-2 and CDK-2?

<p>Their selectivity models (D)</p>
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What is the problem that was solved in the development of an analog-friendly route?

<p>Incorporation of a chiral amine (C)</p>
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What is the role of BINAP in the synthesis of 2-Phenyl Pyridines?

<p>A ligand for the palladium catalyst (B)</p>
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What is the purpose of the mCPBA step in the development of an analog-friendly route?

<p>To form a sulfoxide bond (D)</p>
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What is the characteristic of the synthesis route described?

<p>Scaleable synthesis with little/no chromatography (B)</p>
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